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In vitro and in vivo efficacies of the new triazole albaconazole against Cryptococcus neoformans.

Abstract
The activity of albaconazole (UR-9825; J. Uriach & Cía. S.A., Barcelona, Spain) was compared to that of fluconazole against 12 isolates of Cryptococcus neoformans in vitro and against 1 isolate in vivo in a rabbit model of cryptococcal meningitis. Albaconazole was 100-fold more potent in vitro than fluconazole on a per-weight basis and was fungicidal at potentially relevant concentrations for two isolates. MICs ranged from </=0.0012 to 1.25 micro g/ml, with the MICs for most isolates being between 0.039 and 0.156 micro g/ml. Isolates were from human immunodeficiency virus (HIV)-infected and non-HIV-infected patients and were of serotypes A, B, and C; and the fluconazole MICs for some of the isolates were elevated. Infected rabbits were treated with either fluconazole or albaconazole at dosages ranging from 5 to 80 mg/kg of body weight/day. The peak concentrations of albaconazole in serum and cerebrospinal fluid (CSF) averaged 4.14 and 0.62 micro g/ml, respectively, in animals receiving 80 mg/kg/day. Comparison of the concentrations in serum and CSF suggested a level of CSF penetration of approximately 15%. Despite limited penetration into the subarachnoid space, at all three doses tested albaconazole was as effective as fluconazole for the treatment of cryptococcal meningitis in rabbits.
AuthorsJ L Miller, W A Schell, E A Wills, D L Toffaletti, M Boyce, D K Benjamin Jr, J Bartroli, J R Perfect
JournalAntimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 48 Issue 2 Pg. 384-7 (Feb 2004) ISSN: 0066-4804 [Print] United States
PMID14742184 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Antifungal Agents
  • Quinazolines
  • Triazoles
  • Fluconazole
  • albaconazole
Topics
  • Animals
  • Antifungal Agents (pharmacology, therapeutic use)
  • Colony Count, Microbial
  • Cryptococcus neoformans (drug effects)
  • Fluconazole (therapeutic use)
  • Meningitis, Cryptococcal (drug therapy, microbiology)
  • Microbial Sensitivity Tests
  • Quinazolines (pharmacology, therapeutic use)
  • Rabbits
  • Survival Analysis
  • Triazoles (pharmacology, therapeutic use)

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